EA200901402A1 - THERAPEUTICOL AGAINST GLAUCOMA, CONTAINING AS Adenosine Derivative as an Active Ingredient - Google Patents

THERAPEUTICOL AGAINST GLAUCOMA, CONTAINING AS Adenosine Derivative as an Active Ingredient

Info

Publication number
EA200901402A1
EA200901402A1 EA200901402A EA200901402A EA200901402A1 EA 200901402 A1 EA200901402 A1 EA 200901402A1 EA 200901402 A EA200901402 A EA 200901402A EA 200901402 A EA200901402 A EA 200901402A EA 200901402 A1 EA200901402 A1 EA 200901402A1
Authority
EA
Eurasian Patent Office
Prior art keywords
group
cycloalkyl
glaucoma
hydrogen atom
therapeuticol
Prior art date
Application number
EA200901402A
Other languages
Russian (ru)
Other versions
EA015971B1 (en
Inventor
Ацуси Симазаки
Норико Кавабата
Томоко Кирихара
Джейсон М. Риджер
Роберт Д. Томпсон
Original Assignee
Сантен Фармасьютикал Ко., Лтд.
ПГэксХЕЛТ, ЛЛК
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Сантен Фармасьютикал Ко., Лтд., ПГэксХЕЛТ, ЛЛК filed Critical Сантен Фармасьютикал Ко., Лтд.
Publication of EA200901402A1 publication Critical patent/EA200901402A1/en
Publication of EA015971B1 publication Critical patent/EA015971B1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/167—Purine radicals with ribosyl as the saccharide radical

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Изобретение относится к терапевтическому средству против глаукомы. Соединение общей формулы (1) или его соль обнаруживают превосходное понижающее действие на внутриглазное давление в испытании на снижение внутриглазного давления и применимы в качестве профилактического или терапевтического средства против глаукомы или глазной гипертензии.В указанной формуле Х представляет собой СН или N; Rпредставляет собой атом водорода, гидроксигруппу, атом галогена, алкильную группу, алкоксигруппу, циклоалкильную группу, циклоалкоксигруппу, (циклоалкил)алкоксигруппу илиRпредставляет собой атом водорода, алкильную группу, циклоалкильную группу, алкилкарбонильную группу или алкилоксикарбонильную группу; Rи Rявляются одинаковыми или различными и представляют собой атом водорода, гидроксигруппу, атом галогена, алкильную группу, алкоксигруппу, циклоалкильную группу или циклоалкоксигруппу.The invention relates to a therapeutic agent against glaucoma. The compound of general formula (1) or a salt thereof exhibits an excellent lowering effect on intraocular pressure in an intraocular pressure reduction test and is useful as a prophylactic or therapeutic agent for glaucoma or ocular hypertension. In said formula X represents CH or N; R represents a hydrogen atom, a hydroxy group, a halogen atom, an alkyl group, an alkoxy group, a cycloalkyl group, a cycloalkoxy group, a (cycloalkyl) alkoxy group or R represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkylcarbonyl group or an alkyloxycarbonyl group; R and R are the same or different and represent a hydrogen atom, a hydroxy group, a halogen atom, an alkyl group, an alkoxy group, a cycloalkyl group or a cycloalkoxy group.

EA200901402A 2007-04-16 2008-04-14 Therapeutic agent for glaucoma containing adenosine derivative as active ingredient EA015971B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007106915A JP2008266143A (en) 2007-04-16 2007-04-16 Glaucoma remedy containing adenosine derivative as active ingredient
PCT/US2008/004770 WO2008130520A1 (en) 2007-04-16 2008-04-14 Therapeutic agent for glaucoma containing adenosine derivative as active ingredient

Publications (2)

Publication Number Publication Date
EA200901402A1 true EA200901402A1 (en) 2010-04-30
EA015971B1 EA015971B1 (en) 2012-01-30

Family

ID=39875791

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200901402A EA015971B1 (en) 2007-04-16 2008-04-14 Therapeutic agent for glaucoma containing adenosine derivative as active ingredient

Country Status (15)

Country Link
US (2) US20100093770A1 (en)
EP (1) EP2134174A4 (en)
JP (2) JP2008266143A (en)
KR (1) KR20090128495A (en)
CN (1) CN101677544A (en)
AU (1) AU2008241496A1 (en)
BR (1) BRPI0809953A2 (en)
CA (1) CA2684866A1 (en)
EA (1) EA015971B1 (en)
IL (1) IL201418A0 (en)
MX (1) MX2009011076A (en)
NZ (1) NZ580165A (en)
UA (1) UA100376C2 (en)
WO (1) WO2008130520A1 (en)
ZA (1) ZA200906989B (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7985754B2 (en) * 2006-07-17 2011-07-26 Trovis Pharmaceuticals, Llc Selective antagonists of A2A adenosine receptors
ME02608B (en) 2010-01-11 2017-06-20 Inotek Pharmaceuticals Corp Combination, kit and method of reducing intraocular pressure
AU2011230618A1 (en) * 2010-03-26 2012-10-11 Inotek Pharmaceuticals Corporation Adenosine compounds and their use thereof
JP2013523739A (en) 2010-03-26 2013-06-17 イノテック ファーマシューティカルズ コーポレイション Method for reducing intraocular pressure in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs thereof
US20120058983A1 (en) 2010-09-02 2012-03-08 Bayer Pharma Aktiengesellschaft Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension
JP2012180346A (en) * 2011-02-10 2012-09-20 Santen Pharmaceut Co Ltd Aqueous composition having improved drug migration property of hydrophilic drug
RS56150B1 (en) 2012-01-26 2017-11-30 Inotek Pharmaceuticals Corp Anhydrous polymorphs of (2r,3s,4r,5r)-5-(6-(cyclopentylamino)-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl) } methyl nitrate and processes of preparation thereof
JP2016513706A (en) 2013-03-15 2016-05-16 イノテック ファーマシューティカルズ コーポレイション Ophthalmic preparations
WO2017137528A1 (en) 2016-02-12 2017-08-17 Charité - Universitätsmedizin Berlin Adenosine a1 receptor agonist for use in treatment of status epilepticus
KR102007640B1 (en) 2017-11-29 2019-08-07 퓨쳐메디신 주식회사 The pharmaceutical compositions for the prevention and treatment of retinal diseases or optic nerve diseases containing adenosine derivatives

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7378400B2 (en) * 1999-02-01 2008-05-27 University Of Virginia Patent Foundation Method to reduce an inflammatory response from arthritis
US7427606B2 (en) * 1999-02-01 2008-09-23 University Of Virginia Patent Foundation Method to reduce inflammatory response in transplanted tissue
US6322771B1 (en) * 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
SG176313A1 (en) * 2001-10-01 2011-12-29 Univ Virginia Patent Found 2-propynyl adenosine analogs having a2a agonist activity and compositions thereof
EP1663311A2 (en) * 2003-09-12 2006-06-07 Allergan, Inc. Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions
US20050058696A1 (en) * 2003-09-12 2005-03-17 Allergan, Inc. Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions
CA2576826C (en) * 2004-08-02 2014-09-30 University Of Virginia Patent Foundation 2-propynyl adenosine analogs with modified 5'-ribose groups having a2a agonist activity
US7368439B2 (en) * 2005-06-15 2008-05-06 Bar - Ilan University Dinucleoside poly(borano)phosphate derivatives and uses thereof
JP2008285478A (en) * 2007-04-16 2008-11-27 Santen Pharmaceut Co Ltd Therapeutic agent for glaucoma comprising adenosine a2a receptor agonist as effective component

Also Published As

Publication number Publication date
US20100093770A1 (en) 2010-04-15
JP4923141B2 (en) 2012-04-25
CN101677544A (en) 2010-03-24
EP2134174A4 (en) 2011-05-25
AU2008241496A1 (en) 2008-10-30
EA015971B1 (en) 2012-01-30
JP2008266143A (en) 2008-11-06
BRPI0809953A2 (en) 2014-09-23
EP2134174A1 (en) 2009-12-23
IL201418A0 (en) 2010-06-16
JP2010524933A (en) 2010-07-22
NZ580165A (en) 2012-07-27
MX2009011076A (en) 2010-01-20
CA2684866A1 (en) 2008-10-30
ZA200906989B (en) 2010-06-30
UA100376C2 (en) 2012-12-25
WO2008130520A1 (en) 2008-10-30
US20130109646A1 (en) 2013-05-02
KR20090128495A (en) 2009-12-15

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU